1000287-05-7

1000287-05-7 structure

Name: TMC310911
Chemical Name: TMC310911
CAS Number: 1000287-05-7
Molecular Formula: C₃₈H₅₃N₅O₇S₂
Molecular Weight: 755.99
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIV Protease
Create Date: 2020-06-01 16:26:34
Modify Date: 2024-01-06 16:23:59
TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity[1][2].

Name	TMC310911

Description	TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity[1][2].
Related Catalog	Research Areas >> Infection Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Protease
Target	EC50: 2.2-14.2 nM (Wild-type HIV-1)[1]
In Vitro	For a panel of 2,011 recombinant isolates with decreased susceptibility to at least one of the currently approved protease inhibitors (PIs), the FC in TMC310911 EC50 is ≤4 for 82% of isolates and ≤10 for 96% of isolates. The fold change (FC) in TMC310911 EC50 is ≤4 and ≤10 for 72% and 94% of isolates with decreased susceptibility to Darunavir, respectively. In vitro resistance selection (IVRS) performed with r13025, a multiple-PI-resistant recombinant isolate, and TMC310911 selected for mutations L10F, I47V, and L90M (FC in TMC310911 EC50 = 16)[1]. The TMC310911 EC50 values against HIV-1/LAI and HIV-2/ROD in MT4 cells with EC50 values of 14.2 nM and 2 nM, respectively, and HIV-1/LAI and HIV-1/SF2 in PBMCs with EC50 values of 2.2 nM and 2.3 nM, respectively, and HIV-1/BaL in M/M cells with an EC50 value of 13.9 nM. And the corresponding EC90 values ranged from 5.0 to 94.7 nM. The TMC310911 CC50 for MT4 cells is 9.9 μM[1].
References	[1]. Dierynck I, et al. TMC310911, a novel human immunodeficiency virus type 1 protease inhibitor, shows in vitro an improved resistance profile and higher genetic barrier to resistance compared with current protease inhibitors. Antimicrob Agents Chemother. 2011 Dec;55(12):5723-31. [2]. Stellbrink HJ, et al. Antiviral activity, pharmacokinetics, and safety of the HIV-1 protease inhibitor TMC310911, coadministered with ritonavir, in treatment-naive HIV-1-infected patients. J Acquir Immune Defic Syndr. 2014 Mar 1;65(3):283-9.

Molecular Formula	C₃₈H₅₃N₅O₇S₂
Molecular Weight	755.99

56-41-7	108-65-6
56-35-9	64-17-5
67-56-1	108-88-3
141-78-6	1310-73-2
13463-67-7	1333-86-4